Pharmaceutical agents have moved far beyond just the aspirin and heparin that were the mainstays of stroke and interventional therapy as recently as 10 to 15 years ago. Our understanding of the mechanisms of thrombus formation and vascular response to damage as well as our armamentarium has tremendously improved in the past decade. Direct thrombin inhibitors, powerful antiplatelet agents, new fibrinolytic agents, and statins now allow far greater manipulation of the intraprocedural and postprocedural clot cascade and atherogenesis. It is mandatory that current-day interventionists understand the correct and appropriate use of these agents to achieve the desired outcomes of therapy.